Högger P, Rohdewald P
Institut für Pharmazeutische Chemie, Westfälische Wilhelms-Universität, Münster, Germany.
Int J Clin Pharmacol Ther. 1999 Aug;37(8):377-85.
The analgesic efficacy and safety of single oral doses of two centrally acting compounds, the combination of 50 mg tilidine and 4 mg naloxone (Valoron N) and 50 mg tramadol (Tramal), were compared to 25, 50 and 75 mg of the non-steroidal antiinflammatory bromfenac in experimental pain.
It was a placebo-controlled double-blind 6-way crossover study design with 12 human volunteers. Acute pain was generated by electrical tooth pulp stimulation. Treatment effects were determined by recording somatosensory-evoked potentials and by subjective pain rating.
The tilidine/naloxone combination clearly was the most potent medication in this study, followed by bromfenac 75 mg, which produced an early pain relief. Tramadol produced poor analgesia, as did bromfenac 25 and 50 mg. There was no dose-response relationship for bromfenac. Control of plasma levels revealed pronounced interindividual differences in peak plasma concentrations for bromfenac, but not for tramadol. Tilidine/naloxone exerted adverse effects in 9, tramadol in 3 volunteers. Under medication with 25 and 50 mg bromfenac, respectively, only one subject reported adverse effects. No adverse effects were experienced with 75 mg bromfenac or placebo.
The results support previous conclusions about the analgesic efficacy of tilidine/naloxone and tramadol in experimental pain. Moreover, the findings suggest that 75 mg bromfenac might be suitable for fast but short relief of pain of non-inflammatory genesis.
比较单次口服两种中枢作用化合物（50毫克替利定与4毫克纳洛酮的组合制剂（瓦洛隆N）和50毫克曲马多）与25毫克、50毫克和75毫克非甾体抗炎药溴芬酸在实验性疼痛中的镇痛效果和安全性。
这是一项安慰剂对照、双盲、六路交叉研究设计，有12名人类志愿者参与。通过电刺激牙髓产生急性疼痛。通过记录体感诱发电位和主观疼痛评分来确定治疗效果。
在本研究中，替利定/纳洛酮组合显然是最有效的药物，其次是75毫克溴芬酸，它能迅速缓解疼痛。曲马多镇痛效果不佳，25毫克和50毫克溴芬酸也是如此。溴芬酸不存在剂量反应关系。血浆水平监测显示，溴芬酸的血浆峰浓度存在明显的个体差异，而曲马多则没有。9名志愿者服用替利定/纳洛酮后出现不良反应，3名志愿者服用曲马多后出现不良反应。分别服用25毫克和50毫克溴芬酸时，只有一名受试者报告有不良反应。服用75毫克溴芬酸或安慰剂时未出现不良反应。
结果支持先前关于替利定/纳洛酮和曲马多在实验性疼痛中镇痛效果的结论。此外，研究结果表明，75毫克溴芬酸可能适用于快速但短暂缓解非炎性疼痛。
